The first oral PCSK9 inhibitor has been approved!
Merck’s enlicitide (Lipfendra®), a once-daily oral macrocyclic PCSK9 inhibitor, has been approved by the FDA as an adjunct to diet and exercise to reduce LDL cholesterol in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia.
PCSK9 has long been considered one of the most challenging cardiovascular targets for an oral drug. By disrupting the PCSK9–LDL receptor protein–protein interaction, enlicitide (MK-0616) delivers antibody-like LDL-C lowering in a pill.
Find out why enlicitide was selected as the 2023 Drug Hunter Molecule of the Year, including:
- Why PCSK9 is such an important—and difficult—therapeutic target
- How mRNA display technology enabled the discovery of an orally active macrocycle
- Highlights from the compound’s clinical development
Read more on DrugHunter: https://t.co/dmY5VsQTG5
#DrugDiscovery #MedicinalChemistry #hypercholesterolemia #Merck #PCSK9 #enlicitide #DrugHunter